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首页> 外文期刊>Journal of Pharmaceutical and Biomedical Analysis: An International Journal on All Drug-Related Topics in Pharmaceutical, Biomedical and Clinical Analysis >Study on the inhibitory effect of furafylline and troleandomycin in the 7-methoxyresorufin-O-demethylase and nifedipine oxidase activities in hepatic microsomes from four poultry species using high-performance liquid chromatography coupled with fluorescence and ultraviolet detection
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Study on the inhibitory effect of furafylline and troleandomycin in the 7-methoxyresorufin-O-demethylase and nifedipine oxidase activities in hepatic microsomes from four poultry species using high-performance liquid chromatography coupled with fluorescence and ultraviolet detection

机译:使用高效液相色谱法耦合荧光和紫外检测,呋喃西米霉素在肝微粒体中呋树西霉素和三叶蛋白霉素抑制作用及肝微粒体的抑制作用

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摘要

The present study reports the in vitro studies with furafylline and troleandomycin (TAO) as specific inhibitors of activities 7-methoxyresorufin-O-demethylase (MROD) and nifedipine oxidase, catalyzed by cytochrome P450 1 A2 (CYP1 A2) and 3A4 human enzymes, respectively, in hepatic microsomes of quail, duck, turkey and chicken. The results suggest that in chicken and quail the MROD activity is carried out by orthologs CYP1 A4 and 1 A5, meanwhile in duck and turkey by a CYP1 A5 ortholog. The nifedipine oxidase activity is carried out by orthologs of the CYP3A family in the four bird species. The use of furafylline and TAO significantly decreased these activities (P0.05) and suggested that the biotransformation of resorufin methyl ether (RME) may be related to more than one avian ortholog. (C)2018 Elsevier B.V. All rights reserved.
机译:本研究报告了用Furafylline和TaO)的体外研究作为活性7-甲氧基硼酸盐的特异性抑制剂7-甲氧基硼酸盐和硝酸钠氧化酶,分别由细胞色素P4501A2(CYP1 A2)和3A4人酶催化 ,在鹌鹑,鸭,火鸡和鸡的肝微粒体。 结果表明,在鸡肉和鹌鹑中,MROD活性由Orthologs Cyp1 A4和1 A5进行,同时通过CYP1 A5 Ortholog的鸭子和土耳其进行。 硝苯地平氧化酶活性由四只鸟物种中Cyp3a家族的直肠道进行。 Furafylline和TaO的使用显着降低了这些活性(P <0.05),并表明Resorufin甲基醚(RME)的生物转移可能与多于一个禽流心的原因有关。 (c)2018年elestvier b.v.保留所有权利。

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